Eilean Therapeutics LLC

DOVER, Del., April 4, 2024 /PRNewswire/ -- Eilean Therapeutics LLC, a biopharmaceutical company dedicated to discovering and developing best-in-class and first-in-class small molecule inhibitors to target escape mutations in hematologic and solid malignancies, is pleased to announce the clearance from the Human Research Ethics Committee in Australia for lomonitinib (ZE46-0134) allowing the company to proceed with a Phase I clinical trial in relapsed/refractory (R/R) AML. Lomonitinib is a highly potent and selective plan-FLT3/IRAK4 inhibitor that targets clinically relevant FLT3 mutations and putative escape pathways. "This is a major milestone for the Eilean team, as we continue to progress an accelerated development of lomonitinib," stated Iain Dukes, Chief Executive Officer of Eilean Therapeutics. "Given the safety profile, extended half-life and target engagement demonstrated in a healthy volunteer study, we look forward to initiating our clinical trial and testing our approach in R/R AML patients." About Lomonitinib Lomonitinib is a highly potent and selective inhibitor of FLT3 ITD, TKD and other clinically relevant FLT3 mutations, as well as IRAK4. FLT3 mutations are the most frequently identified mutations in AML. There are two main mechanisms of resistance to FLT3 inhibitors: the FLT3-ITD-F691L mutation deemed the "gatekeeper" mutation that confers resistance to all currently approved FLT3 inhibitors and the activation of the IRAK4 escape pathway. Lomonitinib inhibits both resistance mechanisms. About the Phase 1 Clinical Trial The Phase I study will evaluate the safety, tolerability, pharmacokinetics, and anti-tumor activity of lomonitinib as monotherapy in R/R AML patients with FLT3 mutations (ITD, TKD or gatekeeper). The study will include a dose escalation and an expansion phase with up to 60 total participants. Eilean Therapeutics is planning to initiate the study in Q2 2024 across multiple investigative sites in Australia. About Eilean Therapeutics Eilean Therapeutics LLC is a biopharmaceutical company co-founded by OrbiMed, Torrey Pines Investment and Dr John C. Byrd, focused on the discovery and development of best-in-class and first-in-class small molecule inhibitors that target escape mutations in hematologic and solid cancers. The company is utilizing a proprietary hybrid AI (Expert Systems Inc.), leveraging its key partners proprietary data, chem/bio tools, knowledge and expertise to choose highly valuable molecular mechanism of pathology, to rationally design, accelerate discovery and optimize development of best-in-class and first-in-class therapies. Eilean Therapeutics' goal is to utilize its capabilities and platform to become a leader in developing novel breakthrough medicines to maximize the clinical benefit when treating hematologic and solid malignancies. For more information visit Media Contact: Amy Burd CSO [email protected] SOURCE Eilean Therapeutics

ROCKVILLE, Md., March 13, 2024 /PRNewswire/ -- Expert Systems, a leader in AI-enabled drug discovery, proudly announces a significant milestone in partnership with Eilean Therapeutics LLC: the start of Phase 1 trial of balamenib (ZE63-0302), a highly selective inhibitor of the menin–KMT2A binding interaction, under the Clinical Trial Notification (CTN) scheme of the Australian Therapeutics Goods Administration (TGA). "Balamenib has a highly differentiated pre-clinical pro indicates important advantages over molecules in the same class in safety, tolerability and feasibility of outpatient treatment," commented Bill Farley, CBO at Expert Systems. "We are proud that our comprehensive hybrid AI-based platform has helped accelerate the development of a new promising & safe treatment for AML." Supported by Orbimed, Torrey Pines Investment, and Dr. John C. Byrd, Eilean Therapeutics is committed to leading the development of innovative therapies that significantly enhance treatment outcomes in both hematologic and solid malignancies. This effort is bolstered by leveraging Expert Systems' cutting-edge AI platform to speed up the discovery and development process. About Balamenib Balamenib (ZE63-0302) is an oral small molecule inhibitor of the menin-KMT2A interaction. In vitro studies with KMT2Ar specific cell lines and in vivo studies using xenograft models demonstrated that balamenib is a potent menin inhibitor when administered both as a stand-alone agent or in combination with other compounds used for the treatment of r/rAML, in particular with eiletoclax (ZE50-0134), and lomonitinib (ZE46-0134), Eilean Therapeutics' BCL-2 selective inhibitor and pan FLT3/IRAK4 inhibitor, respectively. Balamenib demonstrates improved safety compared to other molecules in the same class, with an absence of QTc prolongation and is neither a substrate nor inducer of cytochrome P450 3A4 metabolism. Furthermore, balamenib shows significantly reduced susceptibility to "hot spot" menin mutations currently being encountered in the clinic with other menin inhibitors. About Expert Systems, Inc. Expert Systems, Inc., an advanced accelerator platform, is equipped with a comprehensive, hybrid AI-based system that covers the entire spectrum of preclinical drug discovery and early development phases. This includes target identification, virtual screening, non-clinical and clinical pharmacology, chemical liability assessment, and toxicology. Utilizing a unique combination of proprietary and public databases, Expert Systems employs specialized software tools to evaluate the intellectual property landscape and construct a competitive drug intelligence strategy to de-risk candidate selection for rapid transition from in silico to first-in-human trials. Expert Systems has been pivotal in establishing seed and Series A companies, organizing and managing over 30 research and development programs across various financial investors and strategic partners in North America, Europe, and Australia. To learn more, visit About Eilean Therapeutics Eilean Therapeutics LLC is a cutting-edge biopharmaceutical company, established through a collaboration between Orbimed, Torrey Pines Investment, and Dr. John C. Byrd, dedicated to the identification of both best-in-class and first-in-class small molecule inhibitors targeting escape mutations in both hematologic and solid cancers. The company harnesses the Expert Systems Inc. hybrid AI platform alongside its key partners' exclusive data, chem-bio platforms, knowledge, and expertise. This enables Eilean Therapeutics to select molecular mechanisms of pathology with high clinical relevance, precisely designing and expediting the discovery and development processes for leading-edge therapies. Eilean Therapeutics is committed to leveraging its unique capabilities and platform to create novel, groundbreaking medicines for patients with hematologic and solid malignancies, marking a new era in targeted cancer therapy. For more information, visit Bill Farley CBO bfarley@expertsystems.inc

ROCKVILLE, Md., March 12, 2024 /PRNewswire/ -- Expert Systems, a leader in AI-enabled drug discovery, announces the expansion of the collaboration with Eilean Therapeutics as it joins its new PTPN2 inhibitor program, which Eilean has recently acquired from Ness Therapeutics Inc (Ness) in an all-equity transaction. "Eilean's lead PTPN2 inhibitor molecules demonstrate exceptional efficacy, selectivity, oral bioavailability and a good safety profile," commended Bill Farley, CBO at Expert Systems. "We're proud to be Eilean's partner & leverage our cutting-edge AI platform to help advance a new pipeline of best-in-class immuno-oncological therapy solutions with an improved safety and tolerability profile." About Eilean Therapeutics' PTPN2 Inhibitor Program Protein tyrosine phosphatase non-receptor type 2 (PTPN2), also known as T cell protein tyrosine phosphatase (TC-PTP), is ubiquitously expressed, primarily in hematopoietic and placental cells. As a critical negative regulator of the JAK-STAT pathway, PTPN2 functions to directly regulate signaling through cytokine receptors, including IFNγ. Thus, enhancing IFNγ sensing and signaling through the inhibition of PTPN2 is a potential therapeutic strategy to improve the efficacy of cancer immunotherapy regimens. About Expert Systems, Inc. Expert Systems, Inc., an advanced accelerator platform, is equipped with a comprehensive, hybrid AI-based system that covers the entire spectrum of preclinical drug discovery and early development phases. This includes target identification, virtual screening, non-clinical and clinical pharmacology, chemical liability assessment, and toxicology. Utilizing a unique combination of proprietary and public databases, Expert Systems employs specialized software tools to evaluate the intellectual property landscape and construct a competitive drug intelligence strategy to de-risk candidate selection for rapid transition from in silico to first-in-human trials. Expert Systems has been pivotal in establishing seed and Series A companies, organizing and managing over 30 research and development programs across various financial investors and strategic partners in North America, Europe, and Australia. To learn more, visit About Eilean Therapeutics Eilean Therapeutics LLC is a cutting-edge biopharmaceutical company, established through a collaboration between Orbimed, Torrey Pines Investment, and Dr. John C. Byrd, dedicated to the identification of both best-in-class and first-in-class small molecule inhibitors targeting escape mutations in both hematologic and solid cancers. The company harnesses the Expert Systems Inc. hybrid AI platform alongside its key partners' exclusive data, chem-bio platforms, knowledge, and expertise. This enables Eilean Therapeutics to select molecular mechanisms of pathology with high clinical relevance, precisely designing and expediting the discovery and development processes for leading-edge therapies. Eilean Therapeutics is committed to leveraging its unique capabilities and platform to create novel, groundbreaking medicines for patients with hematologic and solid malignancies, marking a new era in targeted cancer therapy. For more information, visit Media Contact: Bill Farley CBO [email protected] SOURCE Expert Systems, Inc.